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Are tetracaine and lidocaine the same? A Detailed Pharmacological Comparison

4 min read

Over 800,000 prescriptions for lidocaine were issued in the United States in 2023 [1.5.3]. While both are effective local anesthetics, the fundamental question remains for many: are tetracaine and lidocaine the same? The answer lies in their distinct chemical classifications and properties.

Quick Summary

Tetracaine and lidocaine are not the same; they belong to different chemical classes of local anesthetics. Tetracaine is an ester, while lidocaine is an amide, leading to key differences in metabolism, potency, and potential for allergic reactions.

Key Points

  • Not the Same: Tetracaine and lidocaine are different types of local anesthetics; tetracaine is an ester, and lidocaine is an amide [1.3.1].

  • Different Metabolism: Tetracaine is broken down in the blood by plasma esterases, while lidocaine is metabolized by the liver [1.4.7, 1.6.6].

  • Potency and Toxicity: Tetracaine is about four times more potent than lidocaine, but this also corresponds to a higher risk of systemic toxicity [1.6.1, 1.6.2].

  • Allergy Potential: Tetracaine can produce a metabolite (PABA) that is more likely to cause allergic reactions, making lidocaine an alternative for sensitive patients [1.3.3, 1.4.5].

  • Clinical Uses: Lidocaine is widely used for dental work and minor skin procedures, while tetracaine is common in eye drops for ophthalmic procedures and for spinal anesthesia [1.5.4, 1.7.1].

  • Onset and Duration: Both have a rapid onset, but lidocaine generally has an intermediate duration, while tetracaine's duration is highly variable depending on the application [1.5.4, 1.4.8].

  • Combination Therapy: The two are sometimes combined in topical creams to utilize lidocaine's rapid onset and tetracaine's longer duration of action [1.3.3].

In This Article

Understanding Local Anesthetics: The Core Function

Both tetracaine and lidocaine function as local anesthetics by blocking sodium ion channels in nerve endings [1.3.1]. This action prevents the initiation and conduction of nerve impulses, resulting in a temporary loss of sensation or numbness in the targeted area [1.3.1, 1.3.7]. They are used topically on the skin or mucous membranes to prevent pain before minor medical procedures like inserting an IV, drawing blood, or dermatological treatments [1.7.6]. Despite this shared mechanism, their chemical structures dictate significant pharmacological differences.

The Fundamental Difference: Ester vs. Amide

The most critical distinction is that tetracaine is an ester-type local anesthetic, whereas lidocaine belongs to the amide class [1.3.1, 1.3.4]. This chemical variance influences how the body metabolizes each drug.

  • Tetracaine (Ester): Ester anesthetics like tetracaine are metabolized by plasma esterases, which are enzymes found in the blood [1.4.7]. This process is relatively rapid [1.6.2]. A primary metabolite of tetracaine is para-aminobenzoic acid (PABA), which is associated with a higher potential for allergic reactions in some individuals [1.4.5].
  • Lidocaine (Amide): Amide anesthetics such as lidocaine are primarily metabolized in the liver by enzymes like CYP1A2 and CYP3A4 [1.6.6]. This metabolic pathway is different from esters, and as a result, lidocaine is often a suitable alternative for patients with sensitivities to ester-type anesthetics [1.3.3, 1.6.3].

Onset of Action and Duration

While both provide effective anesthesia, their timelines differ, which can influence clinical choices.

  • Lidocaine is known for its rapid onset, often taking effect in under a minute when used for local infiltration and lasting for an intermediate duration of 30 to 120 minutes [1.5.4]. For ophthalmic use via retrobulbar injection, it provides anesthesia for about 1 to 1.5 hours [1.5.2].
  • Tetracaine also has a fast onset, especially for ophthalmic use, where it can take effect in as little as 10-20 seconds [1.4.1, 1.4.3]. However, its duration varies significantly by application. In the eyes, a single application may last only 10-20 minutes, but for spinal anesthesia, it can last for two to three hours [1.4.3, 1.4.8]. In some topical formulations, its effects can be very long-lasting [1.6.2]. When applied for the same duration as a lidocaine-prilocaine mixture, tetracaine has been shown to be more efficacious [1.2.3].

Potency and Toxicity Profile

Potency is a measure of the drug dose required to produce an effect. In this regard, tetracaine is significantly more potent than lidocaine. Tetracaine is considered about four times as potent as lidocaine [1.6.1].

This higher potency also correlates with higher potential toxicity. Systemic toxicity with tetracaine can occur at much lower plasma concentrations compared to lidocaine [1.6.2]. Both drugs can cause central nervous system (CNS) and cardiovascular side effects if excessive amounts are absorbed into the bloodstream. Symptoms can range from dizziness and blurred vision to more severe events like convulsions, respiratory depression, and cardiac arrest [1.6.2]. Due to its higher lipid solubility, tetracaine is one of the most potent, but also more toxic, local anesthetics [1.6.7].

Clinical Applications and Formulations

Both drugs are used extensively, but some applications are more common for one than the other.

  • Lidocaine is one of the most widely used anesthetics in dermatological practices and for minor procedures [1.5.4, 1.7.6]. It's available as injectable solutions, topical creams, gels, sprays, and patches [1.5.3]. It is also used as an antiarrhythmic medication to treat ventricular tachycardia [1.5.3].
  • Tetracaine is commonly used for ophthalmic anesthesia in the form of eye drops due to its rapid onset [1.4.2, 1.7.1]. It is also a component in topical anesthetic creams, often combined with lidocaine (e.g., a 7%/7% cream) to leverage the rapid onset of lidocaine and the prolonged duration of tetracaine [1.3.3]. These combination products are used for dermatological procedures and to numb the skin before needle insertions [1.7.6].
Feature Tetracaine Lidocaine
Drug Class Ester [1.3.4] Amide [1.3.4]
Metabolism Hydrolysis by plasma esterases [1.4.7] Hepatic (Liver) metabolism [1.6.6]
Onset of Action Rapid (e.g., ~15-30 seconds in eyes) [1.4.2] Rapid (e.g., <1 minute for infiltration) [1.5.4]
Duration Variable: Short (10-20 min, ophthalmic) to Long (2-3+ hours, spinal) [1.4.3, 1.4.8] Intermediate (30-120 minutes) [1.5.4]
Potency High (Approx. 4x more potent than lidocaine) [1.6.1] Moderate [1.3.3]
Common Uses Ophthalmic anesthesia (eye drops), spinal anesthesia, topical creams (often in combination) [1.7.1, 1.4.8] Dental procedures, minor skin surgery, topical numbing, antiarrhythmic [1.5.3, 1.5.4]
Allergy Profile Higher potential due to PABA metabolite [1.4.5] Lower potential; alternative for ester allergies [1.3.3]

Conclusion

To answer the question, 'Are tetracaine and lidocaine the same?'—no, they are not. They are distinct local anesthetics belonging to the ester and amide classes, respectively. This core difference dictates their metabolism, potency, duration of action, and clinical applications. Lidocaine is a versatile, rapid-acting amide with a lower allergy risk, while tetracaine is a highly potent, longer-acting ester commonly used in specialized applications like ophthalmology and spinal anesthesia. The choice between them, or their use in combination, depends on the specific medical procedure and patient factors.


Disclaimer: This article is for informational purposes only and does not constitute medical advice. Always consult with a qualified healthcare professional for any health concerns or before making any decisions related to your health or treatment.

For more in-depth information on local anesthetics, you can visit the National Center for Biotechnology Information (NCBI).

Frequently Asked Questions

No, they are in different classes. Tetracaine is an ester-type local anesthetic, and lidocaine is an amide-type local anesthetic [1.3.4].

Tetracaine is significantly more potent than lidocaine, estimated to be about four times as strong [1.6.1].

While a true allergy to lidocaine (an amide) is rare, allergies to tetracaine (an ester) are more common due to its PABA metabolite. A person allergic to an ester anesthetic is not necessarily allergic to an amide anesthetic, making lidocaine a common alternative [1.3.3, 1.4.5].

Tetracaine is used in ophthalmic solutions because it has a very rapid onset of action, taking effect within seconds to numb the eye for procedures or examinations [1.4.1, 1.4.3].

Lidocaine is metabolized primarily in the liver, while tetracaine is metabolized in the blood by enzymes called plasma esterases [1.6.6, 1.4.7].

If absorbed systemically in high amounts, both can cause side effects affecting the central nervous system (like dizziness or seizures) and cardiovascular system (like low blood pressure or irregular heart rate). Tetracaine's toxicity can occur at lower plasma concentrations than lidocaine's [1.6.2].

Yes, they are often combined in topical anesthetic creams. This combination leverages the rapid onset of lidocaine with the longer duration of anesthesia provided by tetracaine [1.3.3].

References

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Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.